Voruciclib

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Voruciclib  纯度: 99.52%

Voruciclib 是一种具有口服活性和选择性 CDK 抑制剂，Ki 为 0.626 nM-9.1 nM。Voruciclib 可以有效阻断 MCL-1 的转录调节子 CDK9。Voruciclib 抑制多种弥漫性大 B 细胞淋巴瘤 (DLBCL) 模型中 MCL-1 的表达。

Voruciclib

Voruciclib Chemical Structure

CAS No. : 1000023-04-0

规格 价格 是否有货 数量
1 mg ￥2800 In-stock
5 mg ￥5500 In-stock
10 mg   询价  
50 mg   询价  

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Voruciclib 相关产品

•相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus

生物活性

Voruciclib is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL)[1].

IC50 & Target[1]

CDK9/cyc T2

0.626 nM (Ki)

CDK9/CycT1

1.68 nM (Ki)

CDK6/cycD1

2.92 nM (Ki)

CDK4/Cyc D1

3.96 nM (Ki)

CDK1/cycB

5.4 nM (Ki)

CDK1/cyc A

9.1 nM (Ki)

体外研究
(In Vitro)

Voruciclib (0.5-5 µM; 6 hours) shows targeted downregulation of MCL-1 in both ABC and GCB subtypes[1].
Ki values for each target such as CDK9/cyc T2, CDK9/cyc T1, CDK6/cyc D1, CDK4/cyc D1, CDK1/cyc B, and CDK1/cyc A for Voruciclib hydrochloride are 0.626 nM, 1.68 nM, 2.92 nM, 3.96 nM, 5.4 nM, 9.1 nM, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: U2932, RIVA, OCI-LY10 cells (ABC subtype), NU-DHL-1, SU-DHL-4, SU-DHL-6 cells (GCB subtype)
Concentration: 0.5 µM, 1 µM, 2 µM, 3 µM, 4 µM, 5 µM
Incubation Time: 6 hours
Result: Showed targeted downregulation of MCL-1 in both ABC and GCB subtypes.

体内研究
(In Vivo)

Combination of Voruciclib hydrochloride (200 mpk; Oral gavage) and Venetoclax (10 mpk, 1 mpk, 50 mpk, 25 mpk in U2932, RIVA, SU-DHL-4 and NU-DHL-1, respectively) leads to enhance tumor growth inhibition compared to either drug alone in U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), and NU-DHL-1 models (five days per week for 3 weeks) of DLBCL[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ABC subtypes (U2932, RIVA, OCI-LY10), GCB subtypes (SU-DHL-4, NU-DHL-1) xenografted in Female NOD.CB17-Prkdcscid/NCrHsd mice
Dosage: 200 mpk
Administration: Oral gavage; U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), OCI-LY10 (six days per week for 2 weeks), NU-DHL-1 (five days per week for 3 weeks)
Result: Enhanced tumor growth inhibition in U2932, RIVA, SU-DHL-4 and NU-DHL-1 models except in OCI-LY10 model.

Clinical Trial

分子量

469.84

Formula

C22H19ClF3NO5
CAS 号

1000023-04-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (106.42 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1284 mL 10.6419 mL 21.2838 mL
5 mM 0.4257 mL 2.1284 mL 4.2568 mL
10 mM 0.2128 mL 1.0642 mL 2.1284 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Dey J, et al. Voruciclib, a clinical stage oral CDK9 inhibitor, represses MCL-1 and sensitizes high-risk Diffuse Large B-cell Lymphoma to BCL2 inhibition. Sci Rep. 2017 Dec 21;7(1):18007.

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